Simeprevir (TMC 435350) is a potent inhibitor of HCV NS3/4A protease (Ki=0.36nM) and viral replication (replicon EC50=7.8nM).
信号通路
Anti-infection; Metabolism; Proteases
靶点
HCV NS3/4A protease
viral replication
-
-
-
IC50
0.36nM(Ki)
7.8nM (EC50)
-
-
-
体外研究
Simeprevir plays an important role in HCV replication. Data from phase I and II clinical trials of TMC-435350 (TMC 435350; TMC 435; TMC-435350) to date have shown that this agent is well tolerated as a once-daily oral therapy and provides potent antiviral activity in HCV genotype 1-infected subjects, with restoration of liver enzymes and no evidence of viral breakthrough.
体内研究
N/A
临床实验
N/A
特征
N/A
相关实验数据(此数据来自于公开文献,信裕生物并不保证其有效性):
酶活性检测实验
方法
N/A
细胞实验
细胞系
N/A
浓度
N/A
处理时间
N/A
方法
N/A
动物实验
动物模型
N/A
配制
N/A
剂量
N/A
给药方式
N/A
参考文献: 1. Raboisson P, et al. Bioorg Med Chem Lett. 2008 Sep 1, 18(17), 4853-8.
2. Lin Tse-I, Lenz Oliver, Fanning Gregory, Verbinnen Thierry, Delouvroy Frederic. Antimicrobial Agents and Chemotherapy. 2009, 53(4), 1377-1385.
3. Xue W, Pan D, Yang Y, Liu H, Yao X. Antiviral Res. 2012 Jan, 93(1), 126-37.
4. Manns M, Reesink H, Berg T, Dusheiko G, Flisiak R, Marcellin P, Moreno C, Lenz O, Meyvisch P, Peeters M, Sekar V, Simmen K, Verloes R. Antivir Ther. 2011, 16(7), 1021-33.
5. Lin TI, Lenz O, Fanning G, Verbinnen T, Delouvroy F, Scholliers A, Vermeiren K, Rosenquist A, Edlund M, Samuelsson B, Vrang L, de Kock H, Wigerinck P, Raboisson P, Simmen K. Antimicrob Agents Chemother. 2009 Apr, 53(4), 1377-85.
包装清单: